- Synthesis and evaluation of anticancer and PDE 5 inhibitory activity of spiro-substituted quinazolin-4-ones
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A series of novel spiro-substituted 2,3-dihydroquinazolin-4(1H)-ones was synthesized and structurally confirmed by spectral analysis, screened for their anticancer activity at a concentration of 10 μΜ against a panel of 56 cell lines derived from nine different types of cancers, including leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, and breast cancers. The synthesized compounds screened for their PDE 5 inhibitory activity and it showed encouraged activity compared to sildenafil. Graphical abstract: [Figure not available: see fulltext.].
- Ameen, Mohamed A.,Ahmed, Essam Kh.,Ramadan, Mohamed,Abd El-Naby, Hisham A.,Abdel-Haseeb, Asmaa A.
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p. 1513 - 1523
(2017/07/18)
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- DIPHENYLBUTYPIPERIDINE AUTOPHAGY INDUCERS
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Autophagy inducing compounds, methods of their preparation and use, and kits containg said compounds are disclosed herein.
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Page/Page column 8; 87-90
(2011/12/02)
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- Facile method for the combinatorial synthesis of 2,2-Disubstituted Quinazolin-4(1 H)-one derivatives catalyzed by iodine in ionic liquids
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A mild and facile method for the combinatorial synthesis of quinazolin-4-(1H)-one derivatives, containing simple 2,2-disubstituted quinazolin-4-(1H)-ones, spirocyclic quinazolin-4-(1H)-ones, spiro-heterocyclic quinazolin-4-(1H)-ones, and dispirocyclic quinazolin-4-(1H)-ones, is described, which results in high yields by using ionic liquids as green media. The method involves the reaction of 2-aminobenzamides with various ketones catalyzed by iodine and provides new quinazolin-4-(1H)-one library for biomedical screening.
- Wang, Xiang-Shan,Yang, Ke,Zhou, Jie,Tu, Shu-Jiang
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scheme or table
p. 417 - 421
(2010/09/05)
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- Synthesis and evaluation as NOP ligands of some spiro[piperidine-4, 2′(1′H)-quinazolin]-4′(3′H)-ones and spiro[piperidine-4,5′(6′H)-[1,2,4]triazolo[1,5-c]quinazolines]
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Some spiro[piperidine-4,2′(1′H)-quinazolin]-4′(3′H) -ones 3 and spiro[piperidine-4,5′(6′H)-[1,2,4]triazolo-1,5-c] quinazolines] 4 were synthesized and evaluated as ligands of the nociceptin receptor. The examined compounds showed partial agonistic activity, except compounds 3, 4n that proved to be pure antagonists.
- Mustazza, Carlo,Borioni, Anna,Sestili, Isabella,Sbraccia, Maria,Rodomonte, Andrea,Ferretti, Rosella,Del Giudice, Maria Rosaria
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p. 611 - 622
(2007/10/03)
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- Synthesis of 1- and 3-(1-substituted 4-piperidinyl)-1,2,3,4-tetrahydro-2-oxoquinazolines as potential antihypertensive agents
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A series of 1- and 3-(1-substituted 4-piperidinyl)-1,2,3,4-tetrahydro-2-oxoquinazolines were synthesized and tested for antihypertensive activity. Among the compounds tested, 1-(2-hydroxy-2-phenethyl)-4-(1,2,3,4-tetrahydro-2-oxo-3-quinazolinyl) piperidine derivatives were generally the most effective in lowering blood pressure in the spontaneous hypertensive rat model. Of these, 1-[2-(4-chlorophenyl)-2-hydroxyethyl]-4-(1,2,3,4-tetrahydro-2-oxo-3- quinazolinyl)piperidine (KF5908) seemed the most promising.
- Takai,Obase,Nakamizo,Teranishi,Kubo,Shuto,Kasuya,Shigenobu,Hashikami,Karashima
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p. 1116 - 1128
(2007/10/02)
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